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Diazepam (Diazepam Tablets) Side Effects, Interactions, Warning


11.16.2018 | Isaac Leapman
Diazepam
Diazepam (Diazepam Tablets) Side Effects, Interactions, Warning

The lower peak concentrations appear due to a slower rate of absorption, with the time required to achieve peak concentrations on average 20 to 25 minutes greater in the presence of antacids. However, this difference was not statistically significant. However, there is no effect on the extent of absorption. Diazepam peak concentrations are 30% lower when antacids are administered concurrently.

A transient syndrome whereby the symptoms that led to treatment with diazepam recur in an enhanced form. This may occur upon discontinuation of treatment. It may be accompanied by other reactions including mood changes, anxiety, and restlessness.

Laboratories : elevated transaminases and alkaline phosphatase.

Central Nervous System: confusion, depression, dysarthria, headache, slurred speech, tremor, vertigo.

It is a colorless crystalline compound, insoluble in water, with the following molecular structure: DIAZEPAM (diazepam) Tablets. Diazepam is a benzodiazepine derivative chemically designated as 7-chloro-1,3-dihydro-1-methyl-5- phenyl-2H-1,4-benzodiazepin-2-one.

In severe cases, the following symptoms may occur: derealization, depersonalization, hyperacusis, numbness and tingling of the extremities, hypersensitivity to light, noise and physical contact, hallucinations or epileptic seizures. Withdrawal symptoms, similar in character to those noted with barbiturates and alcohol have occurred following abrupt discontinuance of diazepam. Generally milder withdrawal symptoms (e.g., dysphoria and insomnia) have been reported following abrupt discontinuance of benzodiazepines taken continuously at therapeutic levels for several months. These withdrawal symptoms may consist of tremor, abdominal and muscle cramps, vomiting, sweating, headache, muscle pain, extreme anxiety, tension, restlessness, confusion and irritability. The more severe withdrawal symptoms have usually been limited to those patients who had received excessive doses over an extended period of time. Consequently, after extended therapy, abrupt discontinuation should generally be avoided and a gradual dosage tapering schedule followed.

In such patients, a 2-fold to 5-fold increase in mean half-life has been reported. Delayed elimination has also been reported for the active metabolite desmethyldiazepam. Decreases in clearance and protein binding, and increases in volume of distribution and half-life has been reported in patients with cirrhosis. Increases in half-life have also been reported in hepatic fibrosis and in both acute and chronic hepatitis (see CLINICAL PHARMACOLOGY : Pharmacokinetics in Special Populations : Hepatic Insufficiency ). Benzodiazepines are commonly implicated in hepatic encephalopathy.

Diazepam is not recommended in the treatment of psychotic patients and should not be employed instead of appropriate treatment.

10 Aluminum Lake. 1 Aluminum Lake and D&C Yellow No. 2 mg - none 5 mg - FD&C Yellow No.6 Aluminum Lake 10 mg - FD&C Blue No.

Some loss of response to the effects of benzodiazepines may develop after repeated use of diazepam for a prolonged time.

In acute alcohol withdrawal, diazepam tablets may be useful in the symptomatic relief of acute agitation, tremor, impending or acute delirium tremens and hallucinosis.

Since diazepam has a central nervous system depressant effect, patients should be advised against the simultaneous ingestion of alcohol and other CNS-depressant drugs during diazepam therapy.

Abrupt withdrawal of diazepam in such cases may also be associated with a temporary increase in the frequency and/or severity of seizures. As with other agents that have anticonvulsant activity, when diazepam is used as an adjunct in treating convulsive disorders, the possibility of an increase in the frequency and/or severity of grand mal seizures may require an increase in the dosage of standard anticonvulsant medication.

NDC bottles of 100 tablets NDC bottles of 500 tablets.

It is a colorless to light yellow crystalline compound, insoluble in water. Diazepam is a benzodiazepine derivative. The molecular formula is C 16 H 13 ClN 2 O and the molecular weight is 284.74. The chemical name of diazepam is 7-chloro-1,3-dihydro-1- methyl-5-phenyl-2H-1,4-benzodiazepin-2-one. The structural formula is as follows:.

Mylan Pharmaceuticals Inc.: Morgantown, WV 26505 U.S.A. Revised: Sep 2015.

There have also been reports that the metabolic elimination of phenytoin is decreased by diazepam.

Dosage should be individualized for maximum beneficial effect. While the usual daily dosages given below will meet the needs of most patients, there will be some who may require higher doses. In such cases dosage should be increased cautiously to avoid adverse effects.

ADULTS: USUAL DAILY DOSE: Management of Anxiety Disorders and Relief of Symptoms of Anxiety Depending upon severity of symptoms—2 mg to 10 mg, 2 to 4 times daily Symptomatic Relief in Acute Alcohol Withdrawal 10 mg, 3 or 4 times during the first 24 hours, reducing to 5 mg, 3 or 4 times daily as needed Adjunctively for Relief of Skeletal Muscle Spasm 2 mg to 10 mg, 3 or 4 times daily Adjunctively in Convulsive Disorders 2 mg to 10 mg, 2 to 4 times daily Geriatric Patients, or in the presence of debilitating disease 2 mg to 2.5 mg, 1 or 2 times daily initially; increase gradually as needed and tolerated PEDIATRIC PATIENTS: Because of varied responses to CNS-acting drugs, initiate therapy with lowest dose and increase as required. Not for use in pediatric patients under 6 months 1 mg to 2.5 mg, 3 or 4 times daily initially; increase gradually as needed and tolerated.

There is a potentially relevant interaction between diazepam and compounds which inhibit certain hepatic enzymes (particularly cytochrome P450 3A and 2C19). At present, this reaction is known to occur with cimetidine, ketoconazole, fluvoxamine, fluoxetine, and omeprazole. Data indicate that these compounds influence the pharmacokinetics of diazepam and may lead to increased and prolonged sedation.

They are available as follows:. The 2 mg tablets are white, round, scored tablets debossed with MYLAN over 271 on one side and the other side being scored.

Protect from light. Store at 20° to 25°C (68° to 77°F).

(see WARNINGS : Pregnancy ).

Diazepam (diazepam) Injection, Solution 5 mg/mL, Ampul, Fliptop Vial.

If diazepam is to be combined with other centrally acting agents, careful consideration should be given to the pharmacology of the agents employed particularly with compounds that may potentiate or be potentiated by the action of diazepam, such as phenothiazines, antipsychotics, anxiolytics/sedatives, hypnotics, anticonvulsants, narcotic analgesics, anesthetics, sedative antihistamines, narcotics, barbiturates, MAO inhibitors and other antidepressants.

Anxiety or tension associated with the stress of everyday life usually does not require treatment with an anxiolytic. Diazepam tablets, USP are indicated for the management of anxiety disorders or for the short-term relief of the symptoms of anxiety.

They are available as follows:. The 5 mg tablets are orange, round, scored tablets debossed with MYLAN over 345 on one side and the other side being scored.

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Diazepam Injection, USP is a sterile, nonpyrogenic solution intended for intramuscular or intravenous administration. pH 6.6 (6.2 to 6.9). Note: Solution may appear colorless to light yellow. Each milliliter (mL) contains 5 mg diazepam; 40% propylene glycol; 10% alcohol; 5% sodium benzoate and benzoic acid added as buffers; and 1.5% benzyl alcohol added as a preservative.

In elderly patients, it is recommended that the dosage be limited to the smallest effective amount to preclude the development of ataxia or oversedation (2 mg to 2.5 mg once or twice daily, initially to be increased gradually as needed and tolerated).

Patients should also be advised that if they become pregnant during therapy or intend to become pregnant they should communicate with their physician about the desirability of discontinuing the drug. The possibility that a woman of childbearing potential may be pregnant at the time of institution of therapy should be considered. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus. In general, the use of diazepam in women of childbearing potential, and more specifically during known pregnancy, should be considered only when the clinical situation warrants the risk to the fetus.

Safety and effectiveness in pediatric patients below the age of 6 months have not been established.

In addition, children born to mothers receiving benzodiazepines on a regular basis late in pregnancy may be at some risk of experiencing withdrawal symptoms during the postnatal period. There may also be nonteratogenic risks associated with the use of benzodiazepines during pregnancy. There have been reports of neonatal flaccidity, respiratory and feeding difficulties, and hypothermia in children born to mothers who have been receiving benzodiazepines late in pregnancy. An increased risk of congenital malformations and other developmental abnormalities associated with the use of benzodiazepine drugs during pregnancy has been suggested.

Abuse and dependence of benzodiazepines have been reported. Diazepam is subject to Schedule IV control under the Controlled Substances Act of 1970. Once physical dependence to benzodiazepines has developed, termination of treatment will be accompanied by withdrawal symptoms. The risk is more pronounced in patients on long-term therapy. Addiction- prone individuals (such as drug addicts or alcoholics) should be under careful surveillance when receiving diazepam or other psychotropic agents because of the predisposition of such patients to habituation and dependence.

Special Senses : blurred vision, diplopia, dizziness Cardiovascular System: hypotension.

If diazepam is to be combined with other psychotropic agents or anticonvulsant drugs, careful consideration should be given to the pharmacology of the agents to be employed - particularly with known compounds that may potentiate the action of diazepam, such as phenothiazines, narcotics, barbiturates, MAO inhibitors and other antidepressants (see DRUG INTERACTIONS ).

Because of isolated reports of neutropenia and jaundice, periodic blood counts and liver function tests are advisable during long-term therapy.

Should this occur, use of the drug should be discontinued. Psychiatric and paradoxical reactions are known to occur when using benzodiazepines (see ADVERSE REACTIONS ). These reactions are more likely to occur in children and the elderly.

A lower dose is recommended for patients with chronic respiratory insufficiency, due to the risk of respiratory depression.

Amnestic effects may be associated with inappropriate behavior. Antegrade amnesia may occur using therapeutic dosages, the risk increasing at higher dosages.

Gastrointestinal System: constipation, nausea, gastrointestinal disturbances.

Breastfeeding is therefore not recommended in patients receiving diazepam. Diazepam passes into breast milk.

They are available as follows:. The 10 mg tablets are green, round, scored tablets debossed with MYLAN over 477 on one side and the other side being scored.

Urogenital System: incontinence, changes in libido, urinary retention.

The prescribers hould be aware of a risk of seizure in association with flumazenil treatment, particularly in long-term benzodiazepine users and in cyclic antidepressant overdose. Patients treated with flumazenil should be monitored for resedation, respiratory depression and other residual benzodiazepine effects for an appropriate period after treatment. Flumazenil, a specific benzodiazepine-receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. Prior to the administration of flumazenil, necessary measures should be instituted to secure airway, ventilation and intravenous access. The complete flumazenil package insert, including CONTRAINDICATIONS, WARNINGS, and PRECAUTIONS, should be consulted prior to use. Caution should be observed in the use of flumazenil in epileptic patients treated with benzodiazepines. Flumazenil is intended as an adjunct to, not as a substitute for, proper management of benzodiazepine overdose.

Diazepam tablets are a useful adjunct for the relief of skeletal muscle spasm due to reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma ), spasticity caused by upper motor neuron disorders (such as cerebral palsy and paraplegia ), athetosis, and stiff-man syndrome.

Reproduction studies in rats showed decreases in the number of pregnancies and in the number of surviving offspring following administration of an oral dose of 100 mg/kg/day (approximay 16 times the MRHD on a mg/m² basis) prior to and during mating and throughout gestation and lactation. No adverse effects on fertility or offspring viability were noted at a dose of 80 mg/kg/day (approximay 13 times the MRHD on a mg/m² basis). In studies in which mice and rats were administered diazepam in the diet at a dose of 75 mg/kg/day (approximay 6 and 12 times, respectively, the maximum recommended human dose on a mg/m² basis) for 80 and 104 weeks, respectively, an increased incidence of liver tumors was observed in males of both species. Pregnancy Category D. The data currently available are inadequate to determine the mutagenic potential of diazepam.

Overdose of benzodiazepines is usually manifested by central nervous system depression ranging from drowsiness to coma. In more serious cases, symptoms may include ataxia, diminished reflexes, hypotonia, hypotension, respiratory depression, coma (rarely), and death (very rarely). In mild cases, symptoms include drowsiness, confusion, and lethargy. Overdose of benzodiazepines in combination with other CNS depressants (including alcohol) may be fatal and should be closely monitored.

Rodent studies have indicated that prenatal exposure to diazepam doses similar to those used clinically can produce long-term changes in cellular immune responses, brain neurochemistry, and behavior. Diazepam has been shown to be teratogenic in mice and hamsters when given orally at daily doses of 100 mg/kg or greater (approximay eight times the maximum recommended human dose or greater on a mg/m² basis). Cleft palate and encephalopathy are the most common and consistently reported malformations produced in these species by administration of high, maternally toxic doses of diazepam during organogenesis.

Side effects most commonly reported were drowsiness, fatigue, muscle weakness, and ataxia. The following have also been reported:.

Concomitant use with alcohol is not recommended due to enhancement of the sedative effect.

NDC bottles of 100 tablets NDC bottles of 500 tablets.

Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.

The risk is increased in those taking concomitant sedatives (including alcohol) and in the elderly. There have been reports of falls and fractures in benzodiazepine users.

As with the management of intentional overdosage with any drug, it should be considered that multiple agents may have been ingested.

Special care must be taken when diazepam is used during labor and delivery, as high single doses may produce irregularities in the fetal heart rate and hypotonia, poor sucking, hypothermia, and moderate respiratory depression in the neonates. With newborn infants it must be remembered that the enzyme system involved in the breakdown of the drug is not yet fully developed (especially in premature infants).

Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function. Metabolites of this drug are known to be substantially excreted by the kidney, and the risk of toxic reactions may be greater in patients with impaired renal function. Extensive accumulation of diazepam and its major metabolite, desmethyldiazepam, has been noted following chronic administration of diazepam in healthy elderly male subjects.

Oral diazepam tablets may be used adjunctively in convulsive disorders, although it has not proved useful as the sole therapy.

Diazepam Tablets, USP are available containing 2 mg, 5 mg or 10 mg of diazepam, USP.

Vomiting should be induced (within one hour) if the patient is conscious. General supportive measures should be employed, along with intravenous fluids, and an adequate airway maintained. Gastric lavage should be undertaken with the airway protected if the patient is unconscious. Dialysis is of limited value. If there is no advantage in emptying the stomach, activated charcoal should be given to reduce absorption. Intravenous fluids should be administered. Special attention should be paid to respiratory and cardiac function in intensive care. Should hypotension develop, treatment may include intravenous fluid therapy, repositioning, judicious use of vasopressors appropriate to the clinical situation, if indicated, and other appropriate countermeasures. Following overdose with oral benzodiazepines, general supportive measures should be employed including the monitoring of respiration, pulse, and blood pressure.

Psychiatric and Paradoxical Reactions : stimulation, restlessness, acute hyperexcited states, anxiety, agitation, aggressiveness, irritability, rage, hallucinations, psychoses, delusions, increased muscle spasticity, insomnia, sleep disturbances, and nightmares. They are more likely to occur in children and in the elderly. Inappropriate behavior and other adverse behavioral effects have been reported when using benzodiazepines. Should these occur, use of the drug should be discontinued.

The usual precautions are indicated for severely depressed patients or those in whom there is any evidence of latent depression or anxiety associated with depression, particularly the recognition that suicidal tendencies may be present and protective measures may be necessary.

In debilitated patients, it is recommended that the dosage be limited to the smallest effective amount to preclude the development of ataxia or oversedation (2 mg to 2.5 mg once or twice daily, initially, to be increased gradually as needed and tolerated).

Since the risk of withdrawal phenomena and rebound phenomena is greater after abrupt discontinuation of treatment, it is recommended that the dosage be decreased gradually.

Other: changes in salivation, including dry mouth, hypersalivation.

NDC bottles of 100 tablets NDC bottles of 500 tablets.

Benzodiazepines should be used with extreme caution in patients with a history of alcohol or drug abuse (see Drug Abuse And Dependence ).

Minor changes in EEG patterns, usually low-voltage fast activity, have been observed in patients during and after diazepam therapy and are of no known significance.

The following coloring agents are employed:. In addition to the active ingredient diazepam, each tablet contains the following inactive ingredients: colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, pregelatinized starch (corn) and sodium lauryl sulfate. Diazepam is available for oral administration as tablets containing 2 mg, 5 mg or 10 mg diazepam, USP.

The physician should periodically reassess the usefulness of the drug for the individual patient. The effectiveness of diazepam tablets in long-term use, that is, more than 4 months, has not been assessed by systematic clinical studies.

Chronic use (even at therapeutic doses) may lead to the development of physical dependence: discontinuation of the therapy may result in withdrawal or rebound phenomena.

Skin and Appendages : skin reactions.

Diazepam